硫磺酰亞胺
| 中文名稱 | 硫磺酰亞胺 |
|---|---|
| 中文同義詞 | 化合物 T16941;米哚妥林雜質(zhì)5;硫磺酰亞胺;STAUPRIMIDE,抑制劑;化合物 STAUPRIMIDE;施他普利胺;抑胃酶氨酰U丙基亞胺 |
| 英文名稱 | StaupriMide |
| 英文同義詞 | [9S-(9α,10β,11β,13α)]-N-(2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-1,3-dioxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl)-N-methylbenzamide;N-Benzoyl-7-oxostaurosporine;benzaMide deriv.;Stauprimide;Stauprimide - CAS 154589-96-5 - Calbiochem;Benzamide, N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1,3-dioxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methyl-;Stauprimide-d5;N-((5S,6R,7R,9S)-6-Methoxy-5-methyl-14,16-dioxo-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide |
| CAS號(hào) | 154589-96-5 |
| 分子式 | C35H28N4O5 |
| 分子量 | 584.62 |
| EINECS號(hào) | |
| 相關(guān)類別 | 微生物代謝物;抗生素;Antibiotic;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals;Isotope Labelled Compounds |
| Mol文件 | 154589-96-5.mol |
| 結(jié)構(gòu)式 |  |
硫磺酰亞胺 性質(zhì)
| 密度 | 1.52±0.1 g/cm3(Predicted) |
|---|---|
| 儲(chǔ)存條件 | -20°C |
| 溶解度 | 二甲基亞砜：>20mg/mL |
| 酸度系數(shù)(pKa) | 9.51±0.70(Predicted) |
| 形態(tài) | 黃色固體 |
| 顏色 | 白色至米色 |
| 穩(wěn)定性 | 自購買之日起 2 年內(nèi)保持穩(wěn)定。 DMSO 溶液可在 -20°C 下保存長達(dá) 2 個(gè)月。 |
| InChIKey | MQCCJEYZKWZQHU-RWONCURMNA-N |
| SMILES | C(N([C@@H]1C[C@@]2([H])O[C@@](C)([C@@H]1OC)N1C3=C(C4=C1C1=C(C5=C(N21)C=CC=C5)C1C(=O)NC(=O)C=14)C=CC=C3)C)(=O)C1=CC=CC=C1 |&1:2,4,7,9,r| |
Stauprimide (10 μM; 6 hours) suppresses MYC transcription in the majority of cell lines tested with an EC 50 range of 30 nM-8 μM, and decreases MYC levels between 15% to over 90%. Stauprimide (2-8 μM; 24-72 hours) down-regulates MYC leads to the inhibition of cell proliferation in vitro with an IC 50 of 780 nM in RXF 393 cells. Stauprimide (5 μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation. Stauprimide (4-10 μM; 6 hours) acts with different EC 50 s and with different degrees of maximal MYC mRNA down-regulation in different cell lines.
Cell Proliferation Assay
| Cell Line: | Renal cancer cell line RXF 393 cells |
| Concentration: | 2 μM, 4 μM, 8 μM |
| Incubation Time: | 24 hours, 48 hours, 72 hours |
| Result: | Inhibited cell proliferation at concentrations of 2-8 μM. |
Western Blot Analysis
| Cell Line: | Renal cancer cell line RXF 393 cells and CAKI-1 cells |
| Concentration: | 5 μM |
| Incubation Time: | 3 hours |
| Result: | Decreased nuclear localized NME2. |
RT-PCR
| Cell Line: | CA46 cells; Ramos cells; RXF393 cells; TK10 cells; KG1A cells; CAKI-1 cells |
| Concentration: | 4μM, 6μM, 8μM, 10μM |
| Incubation Time: | 6 hours |
| Result: | Suppressed MYC transcription in KG1A cells with an EC 50 of 400±50 nM and a suppression of 90%; CA46 cells were resistant to stauprimide. |
Stauprimide (oral administration; 50 mg/kg; once daily; 30 days, 55 days) blocks tumor growth, reduces MYC protein levels in xenograft mouse with RXF 393 or CAKI-1 cells and inhibits MYC transcription in the RXF 393 tumor.
| Animal Model: | Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice |
| Dosage: | 50 mg/kg |
| Administration: | Oral administration; 50 mg/kg; once daily; 30 days, 55 days |
| Result: | Blocked tumor growth in mice injected with either RXF 393 or CAKI-1 cells during the dosing periods. |
安全信息
| WGK Germany | 3 |
|---|---|
| 海關(guān)編碼 | 2934999090 |
| 存儲(chǔ)類別 | 11 - 可燃固體 |
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-N6747 | 硫磺酰亞胺 Stauprimide | 154589-96-5 | 1 mg | 2200元 |
| 2024/08/19 | HY-N6747 | Stauprimide | 5 mg | 7000元 |